An inhibitor of T. brucei N-myristoyltransferase (Kiapp = 1.44 nM); ameliorated T. brucei infection in mice at 12.5 mg/kg for four days; less potently inhibits growth of T. cruzi (EC50 = 6.9 µM)

DDD85646 – 5 mg

Brand:
Cayman
CAS:
1215010-55-1
Storage:
-20
UN-No:
Non-Hazardous - /

DDD85646 is a moderately bioavailable pyrazole sulphonamide inhibitor of T. brucei N-myristoyltransferase (TbNMT) with an apparent Ki value of 1.44 nM.{18028} T. brucei is the parasite responsible for human African trypanosomiasis (HAT), also known as African sleeping sickness, and is transmitted through the tsetse fly. DDD85646 administration in mice (12.5 mg/kg for four days) ameliorated T. brucei in an acute mouse model of HAT.{18028} It less potently inhibits growth of T. cruzi (EC50 = 6.9 µM).  

 

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Description

An inhibitor of T. brucei N-myristoyltransferase (Kiapp = 1.44 nM); ameliorated T. brucei infection in mice at 12.5 mg/kg for four days; less potently inhibits growth of T. cruzi (EC50 = 6.9 µM)

Formal name: 2,6-dichloro-4-[2-(1-piperazinyl)-4-pyridinyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-benzenesulfonamide

Synonyms:  IMP-366

Molecular weight: 495.4

CAS: 1215010-55-1

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antiparasitics|Antiprotozoals||Product Type|Biochemicals|Small Molecule Inhibitors|Acyltransferases||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Parasitic Diseases|African Sleeping Sickness||Research Area|Infectious Disease|Parasitic Diseases|Chagas Disease

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